-
British Journal of Pharmacology Oct 19681. Pyridostigmine labelled with carbon-14 in the methyl group of the quaternary nitrogen has been used to investigate the excretion and metabolism of the drug after...
1. Pyridostigmine labelled with carbon-14 in the methyl group of the quaternary nitrogen has been used to investigate the excretion and metabolism of the drug after administration of single doses (500 mug) to the rat by stomach tube.2. Pyridostigmine is slowly excreted in the urine; the maximum excretion occurs between 1-3 hr after administration. In 24 hr 42% of the dose is excreted in urine and 38.4% is present in faeces and intestinal contents.3. The peak concentration of radioactivity in liver and blood occurs about 2 hr after administration.4. About 75% of the radioactivity in urine is present as unchanged pyridostigmine, the remainder as metabolite.5. The results are compared with those previously obtained after oral administration of neostigmine.6. It is concluded that after oral administration the absorption of pyridostigmine is greater and the metabolism substantially less than that of neostigmine.
Topics: Absorption; Animals; Carbon Isotopes; Feces; Intestines; Liver; Male; Neostigmine; Pyridostigmine Bromide; Rats
PubMed: 5687596
DOI: 10.1111/j.1476-5381.1968.tb07064.x -
Muscle & Nerve Jun 1999
Topics: Humans; Neuropsychological Tests; Persian Gulf Syndrome; Pyridostigmine Bromide; Risk Factors
PubMed: 10366219
DOI: 10.1002/(sici)1097-4598(199906)22:6<663::aid-mus2>3.0.co;2-a -
Pakistan Journal of Pharmaceutical... Jul 2012The aim of this study was to design and optimize a prolonged release matrix formulation of pyridostigmine bromide, an effective drug in myasthenia gravis and poisoning...
The aim of this study was to design and optimize a prolonged release matrix formulation of pyridostigmine bromide, an effective drug in myasthenia gravis and poisoning with nerve gas, using hydrophilic - hydrophobic polymers via D-optimal experimental design. HPMC and carnauba wax as retarding agents as well as tricalcium phosphate were used in matrix formulation and considered as independent variables. Tablets were prepared by wet granulation technique and the percentage of drug released at 1 (Y(1)), 4 (Y(2)) and 8 (Y(3)) hours were considered as dependent variables (responses) in this investigation. These experimental responses were best fitted for the cubic, cubic and linear models, respectively. The optimal formulation obtained in this study, consisted of 12.8 % HPMC, 24.4 % carnauba wax and 26.7 % tricalcium phosphate, had a suitable prolonged release behavior followed by Higuchi model in which observed and predicted values were very close. The study revealed that D-optimal design could facilitate the optimization of prolonged release matrix tablet containing pyridostigmine bromide. Accelerated stability studies confirmed that the optimized formulation remains unchanged after exposing in stability conditions for six months.
Topics: Chemistry, Pharmaceutical; Cholinesterase Inhibitors; Delayed-Action Preparations; Drug Stability; Models, Theoretical; Pyridostigmine Bromide; Solubility; Tablets
PubMed: 22713949
DOI: No ID Found -
Drug Development and Industrial Pharmacy Apr 2007Pyridostigmine bromide (PB) sustained-release (SR) pellets were developed by extrusion-spheronization and fluid-bed methods using Taguchi experimental and 2(3) full...
Formulation design of a highly hygroscopic drug (pyridostigmine bromide) for its hygroscopic character improvement and investigation of in vitro/in vivo dissolution properties.
Pyridostigmine bromide (PB) sustained-release (SR) pellets were developed by extrusion-spheronization and fluid-bed methods using Taguchi experimental and 2(3) full factorial design. In vitro studies, the 2(3) full factorial design was utilized to search for the optimal SR pellets with specific release rate at different time intervals (release percent of 2, 6, 12, and 24 hr were 6.24, 33.48, 75.18, and 95.26%, respectively) which followed a zero-order mechanism (n=0.93). The results of moisture absorption by Karl Fischer has shown the optimum SR pellets at 25 degrees C/60% RH, 30 degrees C/65% RH, and 40 degrees C/75% RH chambers from 1 hr-4 weeks, attributing that the moisture absorption was not significantly increased. In the in vivo study, the results of the bioavailability data showed the Tmax (from 0.65+/-0.082 hr-4.82+/-2.12 hr) and AUC0-30 hr (from 734.88+/-230.68 ng/mL.hr-1454.86+/-319.28 ng/mL.hr) were prolonged and increased, as well as Cmax (from 251.87+/-27.51 ng/mL-115.08+/-14.87 ng/mL) was decreased for optimum SR-PB pellets when compared with commercial immediate-release (IR) tablets. Furthermore, a good linear regression relationship (r=0.9943) was observed between the fraction dissolution and fraction absorption for the optimum SR pellets. In this study, the formulation design not only improved the hygroscopic character of PB but also achieved the SR effect.
Topics: Absorption; Analysis of Variance; Animals; Area Under Curve; Biological Availability; Chemistry, Pharmaceutical; Cholinesterase Inhibitors; Delayed-Action Preparations; Drug Stability; Drug Storage; Humidity; Kinetics; Linear Models; Male; Microscopy, Electron, Scanning; Pyridostigmine Bromide; Rabbits; Solubility; Technology, Pharmaceutical
PubMed: 17523005
DOI: 10.1080/03639040601031890 -
International Journal of Environmental... Jan 2022mutations lead to complex neurodevelopmental syndromes, including infantile hypotonia with psychomotor retardation and characteristic facies (IHPRF) and congenital...
mutations lead to complex neurodevelopmental syndromes, including infantile hypotonia with psychomotor retardation and characteristic facies (IHPRF) and congenital contractures of limbs and face, hypotonia, and developmental delay (CLIFAHDD), which are recessively and dominantly inherited, respectively. We present a patient in whom congenital myasthenic syndrome (CMS) was suspected due to the occurrence of hypotonia and apnea episodes requiring resuscitation. For this reason, treatment with pyridostigmine was introduced. After starting the treatment, a significant improvement was observed in reducing the apnea episodes and slight psychomotor progress. In the course of further diagnostics, CMS was excluded, and CLIFAHDD syndrome was confirmed. Thus, we try to explain a possible mechanism of clinical improvement after the introduction of treatment with pyridostigmine in a patient with a mutation in the gene.
Topics: Contracture; Humans; Membrane Proteins; Muscle Hypotonia; Mutation; Pyridostigmine Bromide; Sleep Apnea, Central; Syndrome
PubMed: 35055596
DOI: 10.3390/ijerph19020775 -
Clinical Autonomic Research : Official... Dec 2005
Topics: Follow-Up Studies; Humans; Hypotension, Orthostatic; Pyridostigmine Bromide; Research Design
PubMed: 16362550
DOI: 10.1007/s10286-005-0321-4 -
Oral Diseases Oct 2009Pemphigus vulgaris (PV) is an autoimmune blistering disease affecting primarily oral mucosa and skin. Among the drugs used for the therapy of pemphigus, both...
Serum of patients with oral pemphigus vulgaris impairs keratinocyte wound repair in vitro: a time-lapse study on the efficacy of methylprednisolone and pyridostigmine bromide.
OBJECTIVES
Pemphigus vulgaris (PV) is an autoimmune blistering disease affecting primarily oral mucosa and skin. Among the drugs used for the therapy of pemphigus, both methylprednisolone (MP) and pyridostigmine bromide (PBr) can prevent acantholysis in vitro. However, their putative therapeutic properties in regenerating PV-like lesions and promoting the healing process still remain to be demonstrated. To address this issue, here we have developed a model for studying the process of epithelial cleft regeneration in PV by artificially wounding keratinocyte monolayers.
MATERIALS AND METHODS
The experimental model was established by scratching confluent monolayers to simulate the epithelial cleft; then, wound regeneration in the presence of submaximal concentrations of PV sera was studied by time-lapse microscopy, with or without the addition of MP and PBr in the culture medium.
RESULTS
Pemphigus vulgaris serum inhibited epithelial cleft repair of wounded monolayers. Indeed, in the presence of 10% (v/v) PV serum, keratinocytes reached only 2% confluence within 72 h vs an almost complete healing of controls. When administered together with PV sera, MP significantly (P < 0.01) enhanced wound fill by 30% after 72 h. PV-associated wound repair was significantly (P < 0.05) ameliorated by PBr by 24 h and keratinocytes reached 20% confluence after 72 h. Interestingly, neither MP nor PBr could accelerate wound healing when compared with untreated control monolayers.
CONCLUSIONS
In PV, MP and PBr exert their curative effects in part by enhancing the regeneration properties of keratinocytes. Indeed, our data suggest that both drugs can specifically counterbalance the detrimental effects of PV serum on keratinocyte wound healing. These findings provide an explanation for the efficacy of MP and PBr in the treatment of PV lesions in human skin and oral mucosa.
Topics: Cell Line; Cholinergic Agonists; Desmoglein 3; Glucocorticoids; Humans; Keratinocytes; Methylprednisolone; Mouth Diseases; Pemphigus; Pyridostigmine Bromide; Wound Healing
PubMed: 19519621
DOI: 10.1111/j.1601-0825.2009.01574.x -
Journal of Chromatography. B,... Nov 2003An HPLC/MS/MS method was validated for the low level analysis of pyridostigmine bromide (PB) from guinea pig plasma. An advantage of this strong-cation exchange...
An HPLC/MS/MS method was validated for the low level analysis of pyridostigmine bromide (PB) from guinea pig plasma. An advantage of this strong-cation exchange HPLC/MS/MS method was the enhancement of the ESI-MS signal by providing good retention and good peak shape of PB with a mobile phase of 70% acetonitrile. In addition, the use of 70% acetonitrile in the mobile phase allowed the direct injection of the supernant from the protein precipitated extracted sample. The assay was linear from the range of 0.1 to 50 ng/ml using only 25 microl of sample. The precision and accuracy of the assay was better than 9.1 and 113%, respectively.
Topics: Animals; Cholinesterase Inhibitors; Chromatography, High Pressure Liquid; Guinea Pigs; Pyridostigmine Bromide; Reproducibility of Results; Sensitivity and Specificity; Spectrometry, Mass, Electrospray Ionization
PubMed: 14581074
DOI: 10.1016/j.jchromb.2003.08.021 -
International Journal of Pharmaceutics Aug 2002Pyridostigmine bromide (PB) is an anticholinesterase agent whose aqueous solubility is high and which has a short elimination half-life. Its dosage rate in the treatment...
Pyridostigmine bromide (PB) is an anticholinesterase agent whose aqueous solubility is high and which has a short elimination half-life. Its dosage rate in the treatment of myastenia gravis is frequent due to the short half-life and it exhibits side effects. Microparticles designed to deliver a pharmaceutical active ingredient efficiently at the minimum dose and also to enhance stability, reduce side effects and modify drug release were prepared in this study using an acrylic polymer (Eudragit) as the vehicle by the spray-drying technique. The drug was either dissolved or dispersed in the polymeric solution and following the preparation of microparticles using different ratios of ingredients, characterization studies including the determination of shape, particle size distribution, amount loaded, release and stability of PB were performed. The results obtained were compared to those of pure PB. Drug release from microparticles could be modified and was found to depend on the shapes of the microparticles. In vitro evaluation results indicate that the frequent dosage and side effects of pure PB may be reduced with the formulation of microparticles.
Topics: Acrylic Resins; Capsules; Cholinesterase Inhibitors; Crystallography, X-Ray; Excipients; Half-Life; Particle Size; Powders; Pyridostigmine Bromide; Spectrophotometry, Infrared
PubMed: 12176241
DOI: 10.1016/s0378-5173(02)00146-1 -
Journal of Chromatography. B,... Apr 2001A method was developed for the separation and quantification of the insecticide chlorpyrifos (O,O-diethyl-O[3,5,6-trichloro-2-pyridinyl] phosphorothioate), its...
Development of a high-performance liquid chromatographic method for the quantification of chlorpyrifos, pyridostigmine bromide, N,N-diethyl-m-toluamide and their metabolites in rat plasma and urine.
A method was developed for the separation and quantification of the insecticide chlorpyrifos (O,O-diethyl-O[3,5,6-trichloro-2-pyridinyl] phosphorothioate), its metabolites chlorpyrifos-oxon (O,O-diethyl-O[3,5,6-trichloro-2-pyridinyl] phosphate) and TCP (3,5,6-trichloro-2-pyridinol), the anti-nerve agent drug pyridostigmine bromide (PB; 3-dimethylaminocarbonyloxy-N-methyl pyridinium bromide), its metabolite N-methyl-3-hydroxypyridinium bromide, the insect repellent DEET (N,N-diethyl-m-toluamide), and its metabolites m-toluamide and m-toluic acid in rat plasma and urine. The method is based on using solid-phase extraction and high-performance liquid chromatography (HPLC) with reversed-phase C18 column, and gradient UV detection ranging between 210 and 280 nm. The compounds were separated using a gradient of 1-85% acetonitrile in water (pH 3.20) at a flow-rate ranging between 1 and 1.7 ml/min over a period of 15 min. The retention times ranged from 5.4 to 13.2 min. The limits of detection ranged between 20 and 150 ng/ml, while the limits of quantitation were between 150 and 200 ng/ml. Average percentage recovery of five spiked plasma samples was 80.2+/-7.9, 74.9+/-8.5, 81.7+/-6.9, 73.1+/-7.8, 74.3+/-8.3, 80.8+/-6.6, 81.6+/-7.3 and 81.4+/-6.5, and from urine 79.4+/-6.9, 77.8+/-8.4, 83.3+/-6.6, 72.8+/-9.0, 76.3+/-7.7, 83.4+/-7.9, 81.6+/-7.9 and 81.8+/-6.8 for chlorpyrifos, chlorpyrifos-oxon, TCP, pyridostigmine bromide, N-methyl-3-hydroxypyridinium bromide, DEET, m-toluamide and m-toluic acid, respectively. The relationship between peak areas and concentration was linear over a range between 200 and 2000 ng/ml.
Topics: Animals; Calibration; Chlorpyrifos; Cholinesterase Inhibitors; Chromatography, High Pressure Liquid; DEET; Insect Repellents; Pyridostigmine Bromide; Rats
PubMed: 11339298
DOI: 10.1016/s0378-4347(01)00028-7